Literature DB >> 3931647

Distribution of glucuronidation capacity (1-naphthol and morphine) along the rat intestine.

A S Koster, A C Frankhuijzen-Sierevogel, J Noordhoek.   

Abstract

The distribution of glucuronidation capacity along the rat intestine was investigated using mucosal cells, isolated from the small intestine, the caecum, and the colon plus rectum. The glucuronidation capacity for 1-naphthol decreases from 787 +/- 75 (duodenum) to 128 +/- 13 (colon plus rectum) pmoles/min X mg cell protein. The ratio between 1-naphthol and morphine glucuronidation was constant throughout the intestine (7.15 +/- 0.37). The distribution of maximal activity of UDP-glucuronosyltransferase in intestinal cell homogenates follows the same pattern. The maximal activity of UDPglucose dehydrogenase in homogenates corresponds closely to the glucuronidation rate in mucosal cells. The activity of beta-glucuronidase in intestinal cell homogenates is constant along the duodenum and jejunum but increases throughout the terminal ileum, caecum, colon and rectum. Subcellular fractionation studies using marker enzymes indicate that UDPglucose dehydrogenase and beta-glucuronidase are cytosolic enzymes in intestinal mucosal cells. Although UDP-glucuronosyltransferase activity is found in both the mitochondrial and the microsomal fractions, no indications for a mitochondrial localization of this enzyme can be found. Activity in the mitochondrial fraction appears to be due to endoplasmic reticulum, associated with the mitochondrial fraction.

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Year:  1985        PMID: 3931647     DOI: 10.1016/0006-2952(85)90728-2

Source DB:  PubMed          Journal:  Biochem Pharmacol        ISSN: 0006-2952            Impact factor:   5.858


  7 in total

Review 1.  Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model.

Authors:  Xianhua Cao; Seth T Gibbs; Lanyan Fang; Heather A Miller; Christopher P Landowski; Ho-Chul Shin; Hans Lennernas; Yanqiang Zhong; Gordon L Amidon; Lawrence X Yu; Duxin Sun
Journal:  Pharm Res       Date:  2006-08       Impact factor: 4.200

2.  Biotransformation enzymes in human intestine: critical low levels in the colon?

Authors:  W H Peters; L Kock; F M Nagengast; P G Kremers
Journal:  Gut       Date:  1991-04       Impact factor: 23.059

3.  Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans.

Authors:  Tae Hwan Kim; Soyoung Shin; Cornelia B Landersdorfer; Yong Ha Chi; Soo Heui Paik; Jayhyuk Myung; Rajbharan Yadav; Stefan Horkovics-Kovats; Jürgen B Bulitta; Beom Soo Shin
Journal:  AAPS J       Date:  2015-05-20       Impact factor: 4.009

4.  Absorption and presystemic glucuronidation of 1-naphthol in the vasculary fluorocarbon emulsion perfused rat small intestine: the influence of the luminal flow rate and intraluminal binding.

Authors:  M H de Vries; G A Hofman; A S Koster; J Noordhoek
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-11       Impact factor: 3.000

5.  Conjugation of 1-naphthol in human gastric epithelial cells.

Authors:  P Déchelotte; M Varrentrapp; H J Meyer; M Schwenk
Journal:  Gut       Date:  1993-02       Impact factor: 23.059

6.  Involvement of the rat gut epithelial and muscular layer, and microflora in chiral inversion and acyl-glucuronidation of R-fenoprofen.

Authors:  S Sattari; F Jamali
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1997 Apr-Jun       Impact factor: 2.569

7.  Morphine induces changes in the gut microbiome and metabolome in a morphine dependence model.

Authors:  Fuyuan Wang; Jingjing Meng; Li Zhang; Timothy Johnson; Chi Chen; Sabita Roy
Journal:  Sci Rep       Date:  2018-02-26       Impact factor: 4.379

  7 in total

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